NSD

NSD製品

All (8)
NSD阻害剤 (6)
NSD拮抗剤(1)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S7110	(+)-JQ1	(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Nat Immunol, 2024, 25(9):1580-1592 Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Commun, 2024, 15(1):4485
S7360	Birabresib (OTX015)	Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Gastroenterology, 2024, S0016-5085(24)00062-3 Sci Rep, 2024, 14(1):9284 J Autoimmun, 2023, 138:103053
S8006	BIX 01294	BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.	Acta Pharm Sin B, 2024, 14(3):1187-1203 Cell Commun Signal, 2024, 22(1):402 Dev Cell, 2023, 58(6):506-521.e5
S8344	AZD5153 6-hydroxy-2-naphthoic acid	AZD5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.	J Immunother Cancer, 2023, 11(4)e006070 J Immunother Cancer, 2023, 11(4)e006070 Res Sq, 2023, 10.21203/rs.3.rs-3314138/v1
S7853	Pelabresib (CPI-0610)	Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Inflammation, 2022, 45(3):1388-1401 Inflammation, 2022, 45(3):1388-1401 Mol Cancer Ther, 2021, 20(4):691-703
E1520^New	NSC 663284	NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain.
E1059	UNC6934	UNC6934 is a a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. UNC6934 is a potent antagonist of NSD2-PWWP1 with a Kd (SPR) of 80 nM and is selective for NSD2-PWWP1 over 14 other PWWP domains including NSD3-PWWP1 UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 μM.
E1613^New	UNC8153	UNC8153 is a selective degrader of nuclear receptor-binding SET domain-containing 2 (NSD2) with a binding Kd of 24 nM, effectively reducing NSD2 protein levels and the dimethylate lysine 36 of histone 3 (H3K36me2) chromatin mark. Its simple warhead promotes proteasome-dependent degradation of NSD2 via a novel mechanism.
S7110	(+)-JQ1	(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Nat Immunol, 2024, 25(9):1580-1592 Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Commun, 2024, 15(1):4485
S7360	Birabresib (OTX015)	Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Gastroenterology, 2024, S0016-5085(24)00062-3 Sci Rep, 2024, 14(1):9284 J Autoimmun, 2023, 138:103053
S8006	BIX 01294	BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.	Acta Pharm Sin B, 2024, 14(3):1187-1203 Cell Commun Signal, 2024, 22(1):402 Dev Cell, 2023, 58(6):506-521.e5
S8344	AZD5153 6-hydroxy-2-naphthoic acid	AZD5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.	J Immunother Cancer, 2023, 11(4)e006070 J Immunother Cancer, 2023, 11(4)e006070 Res Sq, 2023, 10.21203/rs.3.rs-3314138/v1
S7853	Pelabresib (CPI-0610)	Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Inflammation, 2022, 45(3):1388-1401 Inflammation, 2022, 45(3):1388-1401 Mol Cancer Ther, 2021, 20(4):691-703
E1520^New	NSC 663284	NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain.
E1059	UNC6934	UNC6934 is a a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. UNC6934 is a potent antagonist of NSD2-PWWP1 with a Kd (SPR) of 80 nM and is selective for NSD2-PWWP1 over 14 other PWWP domains including NSD3-PWWP1 UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 μM.
E1520^New	NSC 663284	NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain.
E1613^New	UNC8153	UNC8153 is a selective degrader of nuclear receptor-binding SET domain-containing 2 (NSD2) with a binding Kd of 24 nM, effectively reducing NSD2 protein levels and the dimethylate lysine 36 of histone 3 (H3K36me2) chromatin mark. Its simple warhead promotes proteasome-dependent degradation of NSD2 via a novel mechanism.

NSD阻害剤の選択性比較